Department of Fiber Science & Apparel Design, College of Human Ecology, Cornell University, Ithaca, NY 14853, United States.
Int J Pharm. 2020 Jun 30;584:119395. doi: 10.1016/j.ijpharm.2020.119395. Epub 2020 May 11.
Production of electrospun nanofibrous mats of cyclodextrin inclusion complexes with the incorporation of drug molecules would enable promising designing of fast dissolving delivery systems (FDDS) for oral treatments. Here, the single-step electrospinning technique has been applied to prepare cyclodextrin inclusion complex nanofibrous mats (CD-IC NM) of ferulic acid from complete aqueous systems without using any polymeric matrix. The free-standing ferulic acid/CD-IC NM have been electrospun from two different modified cyclodextrin derivatives of hydroxypropyl-beta-cyclodextrin (HP-β-CD) and hydroxypropyl-gamma-cyclodextrin (HP-γ-CD). The initial content of ferulic acid (1/1 ferulic acid/CD (molar ratio) and ~11% (w/w)) has been protected in case of both ferulic acid/CD-IC NM and so the electrospun nanofibrous mats have been fabricated by the ~100% loading efficiency. It has been detected from the in vitro release and disintegration tests that, the amorphous state of ferulic acid based on inclusion complex formation, and the highly porous feature and high surface area of nanofibrous mats have ensured the fast dissolution/release of ferulic acid and disintegration of nanofibrous mats into the liquid medium and artificial saliva. Herein, HP-γ-CD has formed inclusion complexes with ferulic acid more favorably than HP-β-CD and this has leaded to the existence of some un-complexed ferulic acid crystals in ferulic acid/HP-β-CD-IC NM while, ferulic acid has been completely complexed and is in amorphous state in ferulic acid/HP-γ-CD-IC NM. Furthermore, the thermal stability of ferulic acid has been enhanced as an inclusion complexation aid observed by the shift of thermal degradation temperature of ferulic acid from the range of ~120-200 °C to ~140-280 °C.
将药物分子包合到环糊精包合物的电纺纳米纤维垫中,可用于设计快速溶解的口服给药系统(FDDS)。在此,采用单步电纺技术,从完全的水性体系中制备了包含阿魏酸的环糊精包合物纳米纤维垫(CD-IC NM),而无需使用任何聚合物基质。从两种不同的羟丙基-β-环糊精(HP-β-CD)和羟丙基-γ-环糊精(HP-γ-CD)改性环糊精衍生物中,以自由站立的方式电纺出阿魏酸/CD-IC NM。在两种情况下,都保护了阿魏酸的初始含量(1/1 摩尔比的阿魏酸/CD)和11%(w/w),因此电纺纳米纤维垫的负载效率约为 100%。从体外释放和崩解试验中可以检测到,基于包合形成的阿魏酸无定形状态、纳米纤维垫的高多孔特性和高表面积,确保了阿魏酸的快速溶解/释放以及纳米纤维垫在液体介质和人工唾液中的崩解。在此,HP-γ-CD 比 HP-β-CD 更有利于形成阿魏酸包合物,这导致在阿魏酸/HP-β-CD-IC NM 中存在一些未复合的阿魏酸晶体,而阿魏酸则完全被包合并处于无定形状态在阿魏酸/HP-γ-CD-IC NM 中。此外,作为包合辅助剂,观察到阿魏酸的热稳定性得到增强,其热降解温度从120-200°C 范围移动到~140-280°C。